GDC-0425 HCl | CAS#1778671-05-8 | CHK inhibitor| MedKoo

MedKoo Cat#: 575837 | Name: GDC-0425 HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

GDC-0425, also known as RG 7602, is a Checkpoint Kinase 1 inhibitor. GDC-0425 selectively binds to chk1, thereby preventing activity of chk1 and abrogating the repair of damaged DNA. This may lead to an accumulation of damaged DNA, inhibition of cell cycle arrest, and induction of apoptosis. GDC-0425 may potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapeutic agents.

Chemical Structure

GDC-0425 HCl

CAS#1778671-05-8 (2HCl)

Theoretical Analysis

MedKoo Cat#: 575837

Name: GDC-0425 HCl

CAS#: 1778671-05-8 (2HCl)

Chemical Formula: C18H21Cl2N5O

Exact Mass: 321.1590

Molecular Weight: 394.30

Elemental Analysis: C, 54.83; H, 5.37; Cl, 17.98; N, 17.76; O, 4.06

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

1778671-05-8 (2HCl) 1200129-48-1 (free base) 1627539-18-7 (free base)

Synonym

GDC-0425 HCl; GDC 0425; GDC0425; RG-7602; RG 7602; RG7602

IUPAC/Chemical Name

9H-Pyrrolo(2,3-b:5,4-c')dipyridine-6-carbonitrile, 5-((1-ethyl-4-piperidinyl)oxy)- dihydrochloride

InChi Key

XAQHOBZBBAFJDT-UHFFFAOYSA-N

InChi Code

InChI=1S/C18H19N5O.2ClH/c1-2-23-8-5-12(6-9-23)24-17-14(10-19)21-11-15-16(17)13-4-3-7-20-18(13)22-15;;/h3-4,7,11-12H,2,5-6,8-9H2,1H3,(H,20,22);2*1H

SMILES Code

N#CC1=NC=C2C(C3=CC=CN=C3N2)=C1OC4CCN(CC)CC4.[H]Cl.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 394.30 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Takahashi RH, Halladay JS, Siu M, Chen Y, Hop CE, Khojasteh SC, Ma S. Novel Mechanism of Decyanation of GDC-0425 by Cytochrome P450. Drug Metab Dispos. 2017 May;45(5):430-440. doi: 10.1124/dmd.116.074336. Epub 2017 Feb 10. PMID: 28188299. 2: Lee HJ, Cao Y, Pham V, Blackwood E, Wilson C, Evangelista M, Klijn C, Stokoe D, Settleman J. Ras-MEK Signaling Mediates a Critical Chk1-Dependent DNA Damage Response in Cancer Cells. Mol Cancer Ther. 2017 Apr;16(4):694-704. doi: 10.1158/1535-7163.MCT-16-0504. Epub 2017 Jan 30. PMID: 28138032. 3: Infante JR, Hollebecque A, Postel-Vinay S, Bauer TM, Blackwood EM, Evangelista M, Mahrus S, Peale FV, Lu X, Sahasranaman S, Zhu R, Chen Y, Ding X, Murray ER, Schutzman JL, Lauchle JO, Soria JC, LoRusso PM. Phase I Study of GDC-0425, a Checkpoint Kinase 1 Inhibitor, in Combination with Gemcitabine in Patients with Refractory Solid Tumors. Clin Cancer Res. 2017 May 15;23(10):2423-2432. doi: 10.1158/1078-0432.CCR-16-1782. Epub 2016 Nov 4. PMID: 27815358. 4: Ding X, Chen Y, Sahasranaman S, Shi Y, McKnight J, Dean B. A supported liquid extraction LC-MS/MS method for determination of concentrations of GDC-0425, a small molecule Checkpoint kinase 1 inhibitor, in human plasma. Biomed Chromatogr. 2016 Dec;30(12):1984-1991. doi: 10.1002/bmc.3775. Epub 2016 Jul 5. PMID: 27245274.